AM 251
Cat.No:IA3760 Solarbio
CAS:183232-66-8
Molecular Formula:C22H21Cl2IN4O
Molecular Weight:555.24
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥98%
Appearance:White to off-white Solid
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AM 251CAS:183232-66-8
Molecular Formula:C22H21Cl2IN4O
Molecular Weight:555.24
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥98%
Appearance:White to off-white Solid
Qty:
Size:
CAS | 183232-66-8 |
Name | AM 251 |
Molecular Formula | C22H21Cl2IN4O |
Molecular Weight | 555.24 |
Solubility | Soluble in DMSO |
Purity | ≥98% |
Appearance | White to off-white Solid |
Storage | Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
MDL | MFCD01861181 |
SMILES | O=C(C1=NN(C2=CC=C(Cl)C=C2Cl)C(C3=CC=C(I)C=C3)=C1C)NN4CCCCC4 |
InChIKey | BUZAJRPLUGXRAB-UHFFFAOYSA-N |
InChI | InChI=1S/C22H21Cl2IN4O/c1-14-20(22(30)27-28-11-3-2-4-12-28)26-29(19-10-7-16(23)13-18(19)24)21(14)15-5-8-17(25)9-6-15/h5-10,13H,2-4,11-12H2,1H3,(H,27,30) |
PubChem CID | 2125 |
Target Point | Cannabinoid Receptor antagonist |
Passage | GPCR & G Protein;Neuronal Signaling |
Background | AM251 is a selective CB1 receptor antagonist. |
Biological Activity | AM251是选择性大麻素1 (CB1) 受体拮抗剂,IC50 为8 nM。AM251也是 GPR55 的激动剂,EC50为39 nM[1-7]。 |
IC50 | 8nM(CB1 receptor)[1] |
In Vitro | AM251在HEK293细胞中产生激动剂反应,类似于在酵母表达系统中发现的[2]。 AM-251在未受刺激和乙酰化的LDL刺激的Raw 264.7巨噬细胞,CB2 +/+和CB2 - / - 腹膜巨噬细胞中减少胆固醇酯的合成[3]。 |
In Vivo | CB1拮抗剂AM251(3mg/kg,ip)降低辣椒素诱发的夜间行为(F1,18 = 28.45,p <0.0001)。这种抑制作用是基因型依赖的(F1,18 = 14.83,p <0.01),基因型和AM251的作用之间的相互作用接近显著性(F1,18 = 4.704,p = 0.0587)。计划的比较显示,AM251减少了脂肪酸酰胺水解酶(FAAH)KO小鼠中的抗抑郁行为(p <0.01),但相对于它们各自的载体对照,未能改变WT小鼠中的抗抑郁行为(p> 0.2)。 AM251(3mg/kg,ip)减少FAAH KO(F1,9 = 21.43,p <0.01)但不是WT小鼠(p> 0.3)的热超敏反应的持续时间。 AM251在FAAH KO中以时间依赖性方式抑制辣椒素诱发的热超敏反应(F5,9 = 4.349,p <0.01),但在WT小鼠中没有(p> 0.3)。事后分析显示,与FAAH KO动物相比,接受载体(ip)的FAAH KO小鼠在辣椒素后30(p <0.05),60(p <0.05)和90(p <0.001)分钟时显示出增强的热超敏反应。收到AM251)[4]。单向ANOVA显示,与对照相比,注射到大鼠中的AM251(AM-251)显著降低了张开臂中的进入百分比和在张开臂中花费的时间。 Tukey-Kramer测试分析显示,与开放臂中花费的时间相比,对照大鼠的剂量为1mg/kg(P <0.05)和5mg/kg(P <0.01)显著降低。此外,AM251显著降低了开放臂中1和5 mg/kg剂量的百分比(P <0.05)[5]。 |
Animal Experiment | 小鼠[4]在这些实验中使用总共246只体重为17-48g的小鼠。确定基线反应后,小鼠接受单次ip注射(5 mL/kg)AMG9810(3 mg/kg,每组n = 5),AM251(3 mg/kg,每组n = 5)或载体(每组n = 6)。在i.pl.之前30分钟进行Ip注射。辣椒素或载体给药。在皮内注射辣椒素或载体之前和之后10,30,60,90和120分钟评估缩爪潜伏期。在每个时间点在每只爪中一式两份地测量爪撤回潜伏期,并且报告为来自每只动物的两次重复测定的平均值,对受试者进行平均。大鼠[5]使用重量为250-350的雄性Wistar大鼠。使用以下试剂:CB1受体激动剂,Win-55212(0.3,1和5mg/kg,ip); CB1受体拮抗剂,AM251(0.3,1和5mg/kg,ip);在该研究中,内源性大麻素分解抑制剂URB-597(0.03,0.1和0.3mg/kg,ip)。生理盐水(0.9%氯化钠)用作载体。所有药物都是新鲜制备的,并以每10g体重大鼠0.1mL的体积腹膜内(ip)给药。将所有物质溶解在生理盐水中并在升高的迷宫测试前30分钟施用。 |
Kinase Experiment | 在12孔培养板中接种巨噬细胞(2×106 /孔)。在从2mg/mL乙醇储备溶液中加入7-酮胆固醇(7KC)之前1小时,从在DMSO中制备的4mM储备溶液中加入AM-251或SR144528。调节对照以接受等体积的DMSO和乙醇。 16小时后,测定胱天蛋白酶-3活性。所有治疗均一式三份进行,数据以平均RFLU/mg蛋白±SD表示[3]。 |
Data Literature Source | [1]. Bruno A,et al. Beyond radio-displacement techniques for identification of CB1 ligands: the first application of afluorescence-quenching assay. Sci Rep. 2014 Jan 20;4:3757. [2]. Sharir H,et al. Pharmacological characterization of GPR55,a putative cannabinoid receptor. Pharmacol Ther. 2010 Jun;126(3):301-13. [3]. Thewke D,et al. AM-251 and SR144528 are acyl CoA:cholesterol acyltransferase inhibitors. Biochem Biophys Res Commun. 2009 Apr 3;381(2):181-6. [4]. Carey LM,et al. A pro-nociceptive phenotype unmasked in mice lacking fatty-acid amide hydrolase. Mol Pain. 2016 May 13;12. pii: 1744806916649192. [5]. Komaki A,et al. Study the Effect of Endocannabinoid System on Rat Behavior in Elevated Plus-Maze. Basic Clin Neurosci. 2015 Jul;6(3):147-53. [6]. Jiang X,et al. Role of cannabinoid receptor type 1 in tibial and pudendal neuromodulation of bladder overactivity in cats. Am J Physiol Renal Physiol. 2017 Mar 1;312(3):F482-F488. [7]. Sun L,et al. Endocannabinoid activation of CB1 receptors contributes to long-lasting reversal of neuropathic pain by repetitive spinal cord stimulation. Eur J Pain. 2017 May;21(5):804-814. |
Unit | Bottle |
Specification | 5mg 10mg 50mg |
AM251是选择性CB1受体拮抗剂。
Remark:These protocols are for reference only. Solarbio does not independently validate these methods.
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